WO2010129057A8 - Tetracycline compounds - Google Patents

Tetracycline compounds Download PDF

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Publication number
WO2010129057A8
WO2010129057A8 PCT/US2010/001350 US2010001350W WO2010129057A8 WO 2010129057 A8 WO2010129057 A8 WO 2010129057A8 US 2010001350 W US2010001350 W US 2010001350W WO 2010129057 A8 WO2010129057 A8 WO 2010129057A8
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WO
WIPO (PCT)
Prior art keywords
structural formula
tetracycline compounds
compound
variables
directed
Prior art date
Application number
PCT/US2010/001350
Other languages
French (fr)
Other versions
WO2010129057A2 (en
WO2010129057A3 (en
Inventor
Chi-Li Chen
Roger B. Clark
Yonghong Deng
Minsheng He
Louis Plamondon
Cuixiang Sun
Xiao-Yi Xiao
Original Assignee
Tetraphase Pharmaceuticals, Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Tetraphase Pharmaceuticals, Inc. filed Critical Tetraphase Pharmaceuticals, Inc.
Priority to DK10765527.6T priority Critical patent/DK2427425T3/en
Priority to US13/319,298 priority patent/US9315451B2/en
Priority to CN2010800310775A priority patent/CN102459153A/en
Priority to CA2761241A priority patent/CA2761241C/en
Priority to EP10765527.6A priority patent/EP2427425B1/en
Priority to ES10765527.6T priority patent/ES2627772T3/en
Publication of WO2010129057A2 publication Critical patent/WO2010129057A2/en
Publication of WO2010129057A3 publication Critical patent/WO2010129057A3/en
Publication of WO2010129057A8 publication Critical patent/WO2010129057A8/en
Priority to US15/079,926 priority patent/US10072007B2/en
Priority to US15/969,537 priority patent/US20190077803A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/24—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
    • C07C237/26—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton of a ring being part of a condensed ring system formed by at least four rings, e.g. tetracycline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
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    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/04—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms
    • C07C275/20—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton
    • C07C275/24—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing six-membered aromatic rings
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    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/03—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C311/06—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms to acyclic carbon atoms of hydrocarbon radicals substituted by carboxyl groups
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    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C07C311/19—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
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    • C07C51/347—Preparation of carboxylic acids or their salts, halides or anhydrides by reactions not involving formation of carboxyl groups
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    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/06—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
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    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
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    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
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Abstract

The present invention is directed to a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use.
PCT/US2010/001350 2009-05-08 2010-05-07 Tetracycline compounds WO2010129057A2 (en)

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DK10765527.6T DK2427425T3 (en) 2009-05-08 2010-05-07 tetracycline
US13/319,298 US9315451B2 (en) 2009-05-08 2010-05-07 Tetracycline compounds
CN2010800310775A CN102459153A (en) 2009-05-08 2010-05-07 Tetracycline compounds
CA2761241A CA2761241C (en) 2009-05-08 2010-05-07 Tetracycline compounds
EP10765527.6A EP2427425B1 (en) 2009-05-08 2010-05-07 Tetracycline compounds
ES10765527.6T ES2627772T3 (en) 2009-05-08 2010-05-07 Tetracycline compounds
US15/079,926 US10072007B2 (en) 2009-05-08 2016-03-24 Tetracycline compounds
US15/969,537 US20190077803A1 (en) 2009-05-08 2018-05-02 Tetracycline compounds

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US21575709P 2009-05-08 2009-05-08
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SG10201806714PA (en) 2008-08-08 2018-09-27 Tetraphase Pharmaceuticals Inc C7-fluoro substituted tetracycline compounds
US9315451B2 (en) 2009-05-08 2016-04-19 Tetraphase Pharmaceuticals, Inc. Tetracycline compounds
NO2470500T3 (en) 2009-08-28 2018-03-03
JP6301335B2 (en) * 2012-08-31 2018-03-28 テトラフェース ファーマシューティカルズ，インコーポレイテッド Tetracycline compound
AU2017208574B2 (en) * 2016-01-22 2022-09-22 Sandoz Ag Crystalline eravacycline bis-hydrochloride
WO2018045084A1 (en) * 2016-08-30 2018-03-08 Tetraphase Pharmaceuticals, Inc. Tetracycline compounds and methods of treatment
EP3529236B1 (en) 2016-10-19 2024-02-07 Tetraphase Pharmaceuticals, Inc. Crystalline forms of eravacycline
CN110156624B (en) * 2019-05-29 2022-03-08 河北冀衡药业股份有限公司 Method for synthesizing minocycline and derivatives thereof
CN114014756B (en) * 2021-12-24 2023-09-19 青岛科技大学 Preparation method of 3-hydroxy-2-phenyl naphthoate
CN114181078B (en) * 2021-12-24 2023-09-19 青岛科技大学 Refining method of 3-hydroxy-2-phenyl naphthoate
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WO2010129057A2 (en) 2010-11-11
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